Bianchini Francesca, Fabbrizzi Pierangelo, Menchi Gloria, Raspanti Silvia, Bottoncetti Anna, Passeri Alessandro, Andreucci Elena, Guarna Antonio, Calorini Lido, Pupi Alberto, Trabocchi Andrea
Department of Clinical and Experimental Biomedical Science 'Mario Serio', University of Florence, Viale Morgagni 50, 50134 Florence, Italy.
Department of Chemistry 'Ugo Schiff', University of Florence, Via della Lastruccia 13, 50019 Sesto Fiorentino, Florence, Italy.
Bioorg Med Chem. 2015 Mar 1;23(5):1112-22. doi: 10.1016/j.bmc.2014.12.065. Epub 2015 Jan 13.
Taking advantage of click chemistry, we synthesized triazole-containing RGD peptidomimetics capable of binding to αvβ3 integrin with diverse potency, and selected (125)I-labeled compounds proved to interact in vitro and in vivo with αvβ3 integrin expressed by melanoma cells. Two (125)I-compounds containing either 2-aminobenzimidazole or 2-aminopyridine groups as the arginine bioisostere with the capacity to selectively bind cells of highly expressing αvβ3 melanoma xenografts were found using micro-SPECT imaging studies.
利用点击化学，我们合成了含三唑的RGD拟肽，其能够以不同的亲和力与αvβ3整合素结合，并且经选择的（125）I标记化合物在体外和体内均被证明可与黑色素瘤细胞表达的αvβ3整合素相互作用。使用微型单光子发射计算机断层扫描成像研究发现了两种含（125）I的化合物，它们含有2-氨基苯并咪唑或2-氨基吡啶基团作为精氨酸生物电子等排体，能够选择性地结合高表达αvβ3黑色素瘤异种移植物的细胞。
